Comparative pharmacokinetics between tenofovir disoproxil phosphate and tenofovir disoproxil fumarate in healthy subjects

다국어 초록 (Multilingual Abstract)

Tenofovir is the representative treatment for human immunodeficiency virus and hepatitisB virus infection. This study was conducted to assess the pharmacokinetics (PKs) and safetycharacteristics after a single administration of tenofovir disoproxil phosphate comparedto tenofovir disoproxil fumarate in healthy male subjects. An open-label, randomized,single administration, two-treatment, two-sequence crossover study was conducted in 37healthy volunteers. Serial blood samples were collected up to 72 hours. Non-compartmentalanalysis was used to calculate the PK parameters. The 90% confidence intervals (90% CIs)of the geometric mean ratio (GMR) were calculated for comparing tenofovir disoproxilphosphate to tenofovir disoproxil fumarate. Safety assessments were performed includingclinical laboratory tests, adverse events, etc. during the study. The GMR and 90% CIs were1.0514 (0.9527–1.1603) for Cmax and 1.0375 (0.9516–1.1311) for AUClast, respectively, and bothfell within the conventional bioequivalence range of 0.8–1.25. Both tenofovir salt formswere tolerable. This study demonstrated that tenofovir disoproxil phosphate (292 mg) wasbioequivalent to tenofovir disoproxil fumarate (300 mg).

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